Center for Molecular Diversity in Drug Design, Discovery and Delivery, Department of Chemistry, University of South Florida, Tampa, FL 33620, USA.
J Control Release. 2010 Dec 1;148(2):234-40. doi: 10.1016/j.jconrel.2010.08.016. Epub 2010 Aug 19.
The preparation and properties of poly(vinyl benzoate) nanoparticle suspensions as molecular carriers are described for the first time. These nanoparticles can be formed by nanoprecipitation of commercial poly(vinyl benzoate) in water using Pluronic F68 as surfactant, to create spherical nanostructures measuring 200-250nm in diameter. These nanoparticles are stable in phosphate buffer and blood serum, and only slowly degrade in the presence of esterases. Pluronic F68 stabilizes the nanoparticle and also protects it from enzymatic degradation. Up to 1.6% by weight of a lipid-soluble molecule such as coumarin-6 can be introduced into the nanoparticle during nanoprecipitation, compared to a water-soluble compound (5(6)-carboxyfluorescein) which gave almost no loading. Kinetics experiments in phosphate buffer indicate that 78% of the coumarin-6 was encapsulated within the polymer matrix of the nanoparticle, and the residual 22% of coumarin-6 was surface-bound and quickly released. The nanoparticles are non-toxic in vitro towards human epithelial cells (IC(50)>1000μg/mL) and primary bovine aortic endothelial cells (IC(50)>500μg/mL), and non-bactericidal against a selection of representative test microbes (MIC >250μg/mL). These properties suggest that the poly(vinyl benzoate) nanoparticles may be suitable carriers for molecular delivery of lipophilic small molecules such as pharmaceutical and imaging agents.
首次描述了聚（苯乙烯）纳米粒子悬浮液作为分子载体的制备和性质。这些纳米粒子可以通过在水中使用 Pluronic F68 作为表面活性剂进行商业聚（苯乙烯）的纳米沉淀来形成，从而形成直径为 200-250nm 的球形纳米结构。这些纳米粒子在磷酸盐缓冲液和血清中稳定，并且仅在存在酯酶的情况下缓慢降解。Pluronic F68 稳定纳米粒子并保护其免受酶降解。与水溶性化合物（5(6)-羧基荧光素）相比，在纳米沉淀过程中可以将高达 1.6%重量的脂溶性分子（如香豆素-6）引入纳米粒子中，水溶性化合物几乎没有负载。磷酸盐缓冲液中的动力学实验表明，78%的香豆素-6被包裹在纳米粒子的聚合物基质中，而剩余的 22%的香豆素-6是表面结合的并且很快释放。这些纳米粒子在体外对人上皮细胞（IC（50）>1000μg/mL）和原代牛主动脉内皮细胞（IC（50）>500μg/mL）无毒性，并且对代表性测试微生物（MIC>250μg/mL）没有杀菌作用。这些性质表明，聚（苯乙烯）纳米粒子可能适合作为脂溶性小分子（如药物和成像剂）的分子递送的载体。
